U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Created
by admin
on Thu Jul 06 17:14:12 UTC 2023
Edited
by admin
on Thu Jul 06 17:14:12 UTC 2023
Protein Type RECEPTOR
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
UKK18ES9TF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
5-HYDROXYTRYPTAMINE RECEPTOR 1A
Common Name English
ADRB2RL1
Common Name English
5-HT1A
Common Name English
ADRBRL1
Common Name English
G-21
Common Name English
SEROTONIN RECEPTOR 1A
Common Name English
Code System Code Type Description
UNIPROT
P08908
Created by admin on Thu Jul 06 17:14:17 UTC 2023 , Edited by admin on Thu Jul 06 17:14:17 UTC 2023
PRIMARY
PHAROS
P08908
Created by admin on Thu Jul 06 17:14:17 UTC 2023 , Edited by admin on Thu Jul 06 17:14:17 UTC 2023
PRIMARY
FDA UNII
UKK18ES9TF
Created by admin on Thu Jul 06 17:14:17 UTC 2023 , Edited by admin on Thu Jul 06 17:14:17 UTC 2023
PRIMARY
From To
1_109 1_187
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_10
N 1_11
N 1_24
Related Record Type Details
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
Ki
WEAK INHIBITOR->TARGET
INHIBITOR
Ki
LIGAND->TARGET
Inhibited 56% of the stimulation by 10 micromolare serotonin.
Ki
RADIOLIGAND->TARGET
Kd
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
Ki
INHIBITOR -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
Concentration dependent stimulation of [35S]GTPγS binding by F17464 was observed in 5-HT1a - HeLa cells with a maximal response of 56.9 ± 1 % relative to serotonin 10 μM.
EC50
PARTIAL AGONIST->TARGET
Emax = 68.1% of effect of 1 micromolar of 5-HT.
EC50
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST
Ki
AGONIST -> TARGET
AGONIST -> TARGET
RADIOLIGAND->TARGET
ACTIVATOR -> TARGET
AGONIST -> TARGET
Ki
AGONIST -> TARGET
INHIBITOR -> TARGET
Exhibited antagonism activity at both presynaptic and postsynaptic 5-HT1A receptor sites.
Kd
PARTIAL AGONIST->TARGET
Kd
PARTIAL ANTAGONIST->TARGET
F17464 also partially inhibited [35S]GTPγS binding elicited by 1 μM serotonin with a pIC50 of 6.95 ± 0.03 and a residual 59.8 % stimulation at 10 μM.
IC50
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
LIGAND->TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
The strongest receptor binding affinity for 5-MeO-DiPT is at the 5-HT1A receptor.
AGONIST -> TARGET
SELECTIVE
PARTIAL AGONIST->TARGET
PARTIAL AGONIST->TARGET
Ki
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors
BINDING
PARTIAL AGONIST->TARGET
RADIOLIGAND->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
RADIOLIGAND->TARGET
Kd
RADIOLIGAND->TARGET
AGONIST -> TARGET
PARTIAL AGONIST->TARGET
INHIBITOR -> TARGET
INHIBITOR
Ki
AGONIST -> TARGET
AGONIST -> TARGET
RADIOLIGAND->TARGET
Kd
RADIOLIGAND->TARGET
Kd
INHIBITOR -> TARGET
RADIOLIGAND->TARGET
AGONIST -> TARGET
Ki
LIGAND->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL